公开(公告)号：US08299061B2

公开(公告)日：2012-10-30

申请号：US12961714

申请日：2010-12-07

申请人： Macklin Brian Arnold ,  Thomas James Beauchamp ,  Emily Jane Canada ,  Erik James Hembre ,  Jianliang Lu ,  John Robert Rizzo ,  John Mehnert Schaus ,  Qing Shi

发明人： Macklin Brian Arnold ,  Thomas James Beauchamp ,  Emily Jane Canada ,  Erik James Hembre ,  Jianliang Lu ,  John Robert Rizzo ,  John Mehnert Schaus ,  Qing Shi

IPC分类号： A01N43/00 ,  A61K31/55 ,  C07D403/00 ,  C07D235/02

CPC分类号： C07D487/04

摘要： This invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof; as well as a method for treating obesity, a method for treating diabetes, and a pharmaceutical composition.

摘要翻译： 本发明提供式I化合物或其药学上可接受的盐; 以及用于治疗肥胖症的方法，治疗糖尿病的方法和药物组合物。

公开(公告)号：US08168659B2

公开(公告)日：2012-05-01

申请号：US12441570

申请日：2007-10-22

申请人： David Scott Coffey ,  Jingdan Hu ,  Stacy Jo Keding ,  Joseph Herman Krushinski, Jr. ,  John Mehnert Schaus ,  David Edward Tupper

发明人： David Scott Coffey ,  Jingdan Hu ,  Stacy Jo Keding ,  Joseph Herman Krushinski, Jr. ,  John Mehnert Schaus ,  David Edward Tupper

IPC分类号： A61K31/4439 ,  C07D401/12

CPC分类号： C07D401/12 ,  C07D207/38

摘要： Compounds and pharmaceutical compositions comprising compounds of the Formula as CB1 receptor inverse agonists useful for reducing body weight in mammals, treating cognitive impairment associated with schizophrenia, and mitigating treatment emergent weight gain observed during treatment with antipsychotics.

摘要翻译： 化合物和药物组合物，其包含式为CB1受体反向激动剂的化合物，其可用于减少哺乳动物体内的体重，治疗与精神分裂症相关的认知障碍，以及减轻在用抗精神病药治疗期间观察到的治疗急性体重增加。

公开(公告)号：US20110034484A1

公开(公告)日：2011-02-10

申请号：US12935596

申请日：2009-04-02

申请人： John Mehnert Schaus

发明人： John Mehnert Schaus

IPC分类号： A61K31/506 ,  C07D403/12 ,  A61P3/04 ,  A61P25/18

CPC分类号： C07D403/12

摘要： CB-1 receptor inverse agonist compounds of Formula (I) and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia.

摘要翻译： 式（I）的CB-1受体反式激动剂化合物和用于治疗与精神分裂症相关的肥胖症或认知障碍的药物组合物。

公开(公告)号：US20100120785A1

公开(公告)日：2010-05-13

申请号：US12597255

申请日：2008-05-07

申请人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

发明人： Valentina O. Badescu ,  Anne Marie Camp ,  Barry Peter Clark ,  Michael Philip Cohen ,  Sandra Ann Filla ,  Peter Thaddeus Gallagher ,  Sarah Lynne Hellman ,  Michael Philip Mazanetz ,  Marta Maria Pineiro-Nunez ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  Maria Ann Whatton

IPC分类号： A61K31/497 ,  C07D241/02 ,  A61P25/06

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)═ or N═, provided that at least one of A and B is —N═, n is 1-3, m is 0-3, and R14 are as defined herein.

摘要翻译： 本发明提供式I的选择性5-HT7受体拮抗剂化合物及其在治疗偏头痛，持续性疼痛和焦虑中的用途：其中A和B各自独立地为C（H）=或N =，条件是至少一种 A和B为-N =，n为1-3，m为0-3，R 14如本文所定义。

公开(公告)号：US07384934B2

公开(公告)日：2008-06-10

申请号：US10523147

申请日：2003-07-28

申请人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Yvan LeHuerou ,  Fionna Mitchell Martin ,  Marta Maria Pineiro-Nunez ,  Vincent Patrick Rocco ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  David Edward Tupper

发明人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Yvan LeHuerou ,  Fionna Mitchell Martin ,  Marta Maria Pineiro-Nunez ,  Vincent Patrick Rocco ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  David Edward Tupper

IPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61P25/18

CPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04

摘要： Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or —CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, NO2, CN, COR4, C(O)OR4, CONR5R6, NR5R6, SO2NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyly is unsubstituted or substituted with a phenyl; R4 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I)

公开(公告)号：US6133290A

公开(公告)日：2000-10-17

申请号：US334157

申请日：1999-06-16

申请人： Joseph Herman Krushinski, Jr. ,  John Mehnert Schaus

发明人： Joseph Herman Krushinski, Jr. ,  John Mehnert Schaus

IPC分类号： C07D401/04 ,  C07D455/02 ,  C07D471/04 ,  A61K31/454

CPC分类号： C07D455/02 ,  C07D401/04 ,  C07D471/04

摘要： The present invention relates to a compound of formula I: ##STR1## or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT.sub.1F receptors and inhibiting neuronal protein extravasation in a mammal.

摘要翻译： 本发明涉及式I化合物或其药用酸加成盐; 其可用于激活哺乳动物中的5-HT1F受体并抑制神经元蛋白质外渗。

公开(公告)号：US5998622A

公开(公告)日：1999-12-07

申请号：US112562

申请日：1998-07-09

申请人： Sandra Ann Filla ,  Kirk W. Johnson ,  Lee A. Phebus ,  John Mehnert Schaus

发明人： Sandra Ann Filla ,  Kirk W. Johnson ,  Lee A. Phebus ,  John Mehnert Schaus

IPC分类号： A61P25/04 ,  A61K31/00 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61P25/06 ,  A61P43/00 ,  C07D471/04

CPC分类号： C07D471/04 ,  A61K31/00 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545

摘要： This invention provides 5-HT.sub.1F agonists of Formula I; ##STR1## where A-B, X, and R are as defined in the specification. The invention also encompasses pharmaceutical formulations employing compounds of Formula I as well as methods of treating conditions associated with 5-HT.sub.1F activation employing these compounds or compositions. The invention also provides intermediates useful for the preparation of the compounds of Formula I.

摘要翻译： 本发明提供式I的5-HT1F激动剂; 其中A-B，X和R如说明书中所定义。 本发明还包括使用式I化合物的药物制剂以及使用这些化合物或组合物治疗与5-HT1F活化相关的病症的方法。 本发明还提供了可用于制备式I化合物的中间体。

公开(公告)号：US5708008A

公开(公告)日：1998-01-13

申请号：US619783

申请日：1996-03-20

申请人： James Edmund Audia ,  Bruce Anthony Dressman ,  James Joseph Droste ,  James Erwin Fritz ,  Stephen Warren Kaldor ,  Daniel James Koch ,  Joseph Herman Krushinski, Jr. ,  Jeffrey Scott Nissen ,  Vincent Patrick Rocco ,  John Mehnert Schaus ,  Dennis Charles Thompson

发明人： James Edmund Audia ,  Bruce Anthony Dressman ,  James Joseph Droste ,  James Erwin Fritz ,  Stephen Warren Kaldor ,  Daniel James Koch ,  Joseph Herman Krushinski, Jr. ,  Jeffrey Scott Nissen ,  Vincent Patrick Rocco ,  John Mehnert Schaus ,  Dennis Charles Thompson

IPC分类号： A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P25/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D407/14 ,  C07D409/14 ,  Y02P20/582

摘要： This invention provides novel 5-HT.sub.1F agonists of Formula I ##STR1## where A--B, R, R.sup.1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.

摘要翻译： 本发明提供式I的新型5-HT1F激动剂，其中A-B，R，R 1和X如说明书中所定义，其可用于治疗偏头痛及相关疾病。